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TABLE 1
Pharmacological Selectivity of ABT-102
~IC50(μM) Target
~IC50(μM)
Target
Ligand
Adenosine A1
[3H]DPCPX
> 10
Benzodiazepine Central
[3H]Flunitrazepam
> 10
Adenosine A2A
[3H]CGS 21680
> 10
Benzodiazepine Peripheral
[3H]PK 11195
> 10
Adenosine A3
[125I]AB-MECA
> 10
Ca2+ channel verapamil site
[3H]D 888
> 10
Adrenergic 1
[3H]Prazosin
> 10
K+ channel (volt. dependent) [125I]Dendrotoxin
> 10
Adrenergic 2
[3H]RX821002
> 10
K+ channel (Ca2+ dependent) [125I]Apamin
> 10
Adrenergic 1
[3H](-)CGP 12177
> 10
Na+ channel (Site 2)
[3H]Batrachotoxin
> 10
Adrenergic 2
[3H](-)CGP 12177
> 10
Neurokinin NK1
[125I][Sar9,Met(O2)11]-SP
> 10
Angiotensin AT1
[125I][Sar1,Ile8]-ATII > 10
Neurokinin NK2
[125I]NKA
> 10
Angiotensin AT2
[
Bombesin
125
I]CGP 42112A
125
7
Neurokinin NK3
[
[125I][Tyr4]bombesin > 10
Neuropeptide Y1
[125I]peptide YY
> 10
Bradykinin B2
[3H]NPC 17731
> 10
Neuropeptide Y2
[125I]peptide YY
> 10
Cl- channel
[35S]TBPS
> 10
Neurotensin NT1
[125I]Neurotensin
> 10
CCKA
[3H]Devazepide
> 10
PACAP PAC1
[3H]PACAP1-27
> 10
CCKB
[3H]CCK-8
> 10
Melanocortin MC4
[125I]NDP--MSH
> 10
CCR1
[125I]MIP-1
> 10
Galanin GAL1
[125I]Galanin
> 10
CGRP
[125I]-CGRP
> 10
Galanin GAL2
[125I]Galanin
> 10
Cannabinoid CB1
[3H]Win 55212-2
> 10
Melatonin ML1
[125I]Iodomelatonin
> 10
DA uptake
[3H]GBR 12935
> 10
IL-8B (CXCR2)
[125I]IL-8
> 10
Dopamine D1
[3H]SCH 23390
> 10
TNF
[125I] TNF
> 10
Dopamine D3
[3H]Spiperone
> 10
PDGF
[125I]PDGF BB
> 10
Dopamine D4.4
[3H]Spiperone
> 10
PGI2/IP
[3H] iloprost
> 10
3
> 10
Ligand
I][MePhe ]- D5
3
> 10
Dopamine D5
[ H]SCH 23390
> 10
TXA2/PGH2/TP
[ H]SQ 29548
> 10
Endothelin ETA
[125I]Endothelin-1
> 10
Serotonin 5-HT1A
[3H]8-OH-DPAT
> 10
Endothelin ETB
[125I]Endothelin-1
> 10
Serotonin 5-HT1B
[3H]CYP
> 10
GABA
[3H]GABA
> 10
Serotonin 5-HT2A
[3H]Ketanserin
> 10
Histamine H1
[3H]Pyrilamine
> 10
Serotonin 5-HT2C
[3H]Mesulergine
> 10
Histamine H2
[
Muscarinic M1
125
I]APT
3
> 10
Serotonin 5-HT3
[ H]BRL 43694
> 10
[3H]Pirenzepine
> 10
Serotonin 5-HT5A
[3H]LSD
> 10
Muscarinic M2
[3H]AF-DX384
> 10
Serotonin 5-HT6
[3H]LSD
> 10
Muscarinic M3
[3H]4-DAMP
> 10
Serotonin 5-HT7
[3H]LSD
> 10
Muscarinic M4
[3H]4-DAMP
> 10
Sigma
[3H]DTG
> 10
Muscarinic M5
[3H]4-DAMP
> 10
SKCa
[125I]apamin
> 10
Opioid 
[3H]DADLE
> 10
Somatostatin
[125I]Tyr11-somatostatin
> 10
Opioid 
[3H]U 69593
> 10
VIP1 (VPAC1)
[125I]VIP
> 10
Opioid 
[3H]DAMGO
> 10
Vasopressin V1a
[3H]AVP
> 10
ORL1
[3H]Nociceptin
> 10
ORL1
[3H]Nociceptin
> 10
P2X
[3H],MeATP
> 10
PCP
[3H]-TCP
> 10
P2Y
[35S]dATPS
> 10
PACAP, pituitary adenylyl cyclase-activating protein; DPCPX, 8-cyclopentyl-1,3-dipropylxanthine;
CGS 21680, 2-p-(2-carboxyethyl) phenethylamino-5-N-ethylcarboxamidoadenosine; AB-MECA,
4-aminobenzyl-5-N-methylcarboxamidoadenosine; RX 821002, 2-(2-methoxy-1,4-benzodioxan2yl)-2-imidazoline; CGP-12177, 4-[3-(1,1-dimethylethyl)amino]-2-hydroxypropoxy]-1,3-dihydro2H-benzimidazol-2-one; SCH23390, R-(+)-7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5tetrahydro-1H-3-benzazepine; 4-DAMP, 4-diphenylacetoxy-N-methylpiperidine; DADLE, [DAla2,D-Leu5]-enkephalin; U-69593, (+)-(5,7, 8)-N-methyl-N-[7-(1-pyrrolidinyl)-1oxaspiro[4.5]dec-8-yl]benzeneacetamide; DAMGO, [D-Ala2,N-Me-Phe4,Gly5-ol]-enkephalin;
MeATP, methylene-ATP; 8-OH-DPAT, 8-hydroxy-2-dipropylaminotetralin; CYP, cyanopindolol;
LSD, d-lysergic acid diethylamide; CCK, cholecystokinin; PDGF, platelet-derived growth factor;
NE, norepinephrine; DA, dopamine; VIP, vasoactive intestinal peptide; AVP, arginine
vasopressin; GBR12935, (1-[2-(diphenylmethoxy)ethyl-4-(3-phenylpropyl)-piperazine);
PK11195,1-(2-chloro-phenyl)-N-methyl-N-(1-methylpropyl)-1-isoquinoline carboxamide; TBPS, tbutylbicyclophosphorothionate; CCR, chemokine receptor; ORL, opioid receptor-like; MIP,
macrophage inflammatory protein; APT, aminopotentidine; VPAC, (vasoactive intestinal peptide)
pituitary adenylate cyclase-activating peptide receptor; DTG, 1,3-di-o-tolyguanidine; WIN 552122, (R)-(+)-[2,3-dihydro-5-methyl-3-(4-morpholinylmethyl) pyrrolo-[1,2,3-d,e]-1,4-benzoxazin-6-yl]1-naphthalenyl-methanone; AF DX384, 5,11-dihydro-11-[2-(-[8-dipropylamino)methyl]-1piperidinyl]-ethyl]amino]-carbonyl-6H-pyrido[2,3-b] [1,4]benzodiazepin-6-one;BRL 43694,
granisetron; MDL 105,519, (E)-3-(2-phenyl-2-carboxylethenyl)-4,6-dichloro-1[3H]-indole-2-
carboxylic acid; NPC 17731, D-Arg[Hyp3,D-HypE (transprolyl) 7,Oicc8]bradykinin; Ro41-1049, N(2-aminoethyl)-5-(m-fluorophenyl)-4-thiazole carboxamide HCl; CGP 39653, D,L-(E)-2-amino-4propyl-5-phosphono-3-pentenoic acid; CGP 42112A, N--nicotinoyl-Tyr-(N--CBZ-Arg)-Lys-HisPro-Ile-OH; D 888, verapamil derivative; NDP--MSH, Nle4-D-Phe7--melanocyte stimulating
hormone; SP, substance P; SQ 29548, [1S-[1,2 (5Z),3,4]-7-[3-[[2-[(phenylamino)
carbonyl]hydrazino]methyl]-7-oxabicyclo[2.2.1] hept-2-yl]-5-heptenoic acid.